Patents Assigned to Santaris Pharma A/S
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Patent number: 8470791Abstract: Short oligonucleotides directed against the Apo-B100 gene are provided for modulating the expression of Apo-B100. Methods of using these compounds for modulation of Apo-B100 expression and for the treatment of diseases associated with Apo-B100 expression are provided. The oligonucleotides comprise deoxyribonucleosides and locked nucleic acids.Type: GrantFiled: March 19, 2008Date of Patent: June 25, 2013Assignee: Santaris Pharma A/SInventors: Henrik Frydenlund Hansen, Jens Bo Rode Hansen, Christoph Rosenbohm, Ellen Marie Straarup
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Patent number: 8450291Abstract: The invention relates to oligomeric compounds (oligomers), which target PIK3CA mRNA in a cell, leading to reduced expression of PIK3CA. Reduction of PIK3CA expression is beneficial for the treatment of certain medical disorders, such as hyperproliferative diseases (e.g., cancer). The invention provides therapeutic compositions that include the oligomers and methods for modulating the expression of PIK3CA using the oligomers, including methods of treatment.Type: GrantFiled: November 17, 2010Date of Patent: May 28, 2013Assignee: Santaris Pharma A/SInventor: Maj Hedtjarn
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Patent number: 8450290Abstract: The invention provides the combination use of antisense oligomers targeting androgen receptor mRNA and androgen receptor binding inhibitors that reduce androgen receptor activity for the treatment of androgen receptor related medical disorders, such as cancers, particularly prostate cancers and breast cancers.Type: GrantFiled: November 12, 2010Date of Patent: May 28, 2013Assignees: Enzon Pharmaceuticals, Inc., Santaris Pharma A/SInventors: Jesper Worm, Yixian Zhang
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Patent number: 8440809Abstract: The present invention relates to oligomer compounds (oligomers), which target Hsp27 mRNA in a cell, leading to reduced expression of Hsp27. Reduction of Hsp27 expression is beneficial for the treatment of certain medical disorders, such as cancer. The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of Hsp27 using the oligomers, including methods of treatment.Type: GrantFiled: July 1, 2009Date of Patent: May 14, 2013Assignee: Santaris Pharma A/SInventor: Jesper Worm
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Patent number: 8440637Abstract: The present invention relate to the use of a combination of an inhibitor of miR-122 and an inhibitor of VLDL assembly, for the treatment of HCV, hyperlipidemia and hypercholesterolemia.Type: GrantFiled: October 3, 2008Date of Patent: May 14, 2013Assignee: Santaris Pharma A/SInventor: Joacim Elmén
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Publication number: 20130116309Abstract: Oligonucleotides directed against the hypoxia-inducible factor-1? (HIF-1?) gene are provided for modulating the expression of HIF-1?. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the HIF-1?. Methods of using these compounds for modulation of HIF-1? expression and for the treatment of diseases associated with the hypoxia-inducible factor-1? are provided. Examples of diseases are cancer and pre-eclampsia. The oligonucleotides may be composed of deoxyribonucleosides, a nucleic acid analogue, or Locked Nucleic Acid (LNA) or a combination thereof.Type: ApplicationFiled: December 21, 2012Publication date: May 9, 2013Applicants: Santaris Pharma A/S, Enzon Pharmaceuticals, Inc.Inventors: Enzon Pharmaceuticals, Inc., Santaris Pharma A/S
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Patent number: 8410071Abstract: The present disclosure relates to an LNA oligonucleotide consisting of a sequence selected from the group consisting of 5?-(Tx)GxGxcsasasgscsastscscsTxGxT-3? and 5?-(Gx)TxTxascstsgscscststscsTxTxA-3?, wherein capital letters designate a beta-D-oxy-LNA nucleotide analogue, small letters designate a 2-deoxynucleotide, underline designates either a beta-D-oxy-LNA nucleotide analogue or a 2-deoxynucleotide, subscript “s” designates a phosphorothioate link between neighboring nucleotides/LNA nucleotide analogues, and subscript “x” designates either a phosphorothioate link or a phosphorodiester link between neighboring nucleotides/LNA nucleotide analogues, and wherein the sequence is optionally extended by up to five 2-deoxynucleotide units. The LNA oligonucleotides are useful for modulating the expression of hypoxia-inducible factor-1a (HIF-1a), e.g. in the treatment of cancer diseases, inhibiting angiogenesis, inducing apoptosis, preventing cellular proliferation, or treating an angiogenic disease, e.g.Type: GrantFiled: April 4, 2011Date of Patent: April 2, 2013Assignees: Santaris Pharma a/s, Enzon Pharmaceuticals, Inc.Inventors: Majken Westergaard, Charlotte Albaek Thrue, Frank Winther Rasmussen, Henrik Frydenlund Hansen
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Patent number: 8404659Abstract: The present invention provides compositions and methods of treatment of diseases that are sensitive to drugs that downregulate the function of microRNA's, mRNA, non-coding RNA, or viral genomes. In particular, it has been discovered that a very long term effect of an anti microRNA oligonucleotide may be obtained when administered to a primate. Therefore, the present invention relate to pharmaceutical compositions and methods for treatment of primates, including humans wherein the compositions are administered with a long time interval.Type: GrantFiled: March 9, 2009Date of Patent: March 26, 2013Assignee: Santaris Pharma A/SInventors: Sakari Kauppinen, Niels Abrahamsen, Elisabeth S. Hildebrandt-Eriksen, Martin Munk
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Patent number: 8361980Abstract: The present invention provides compositions and methods of treatment of diseases that are sensitive to drugs that downregulate the function of microRNA's, mRNA, non-coding RNA, or viral genomes. In particular, it has been discovered that a very long term effect of an anti microRNA oligonucleotide may be obtained when administered to a primate. Therefore, the present invention relate to pharmaceutical compositions and methods for treatment of primates, including humans wherein the compositions are administered with a long time interval.Type: GrantFiled: March 9, 2009Date of Patent: January 29, 2013Assignee: Santaris Pharma A/SInventors: Sakari Kauppinen, Niels Abrahamsen, Elisabeth Hildebrandt-Eriksen, Martin Munk
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Publication number: 20120322848Abstract: The present disclosure concerns LNA oligonucleotides having a (sub)sequence of the general formula 5?-(MeCx)(Tx)MeCxAsAstsCsCsastsgsgsMeCxAx(Gx)(c)-3?, and preferably of the general formula 5?-MeCxTxMeCxAsastscscsastsgsgsMeCxAxGxc-3?, wherein capital letters designate an LNA nucleotide analogue selected from ?-D-oxy-LNA, ?-D-thio-LNA, ?-D-amino-LNA and ?-L-oxy-LNA, small letters designate a deoxynucleotide, and underline designates either an LNA nucleotide analogue as defined above or a deoxynucleotide. Such LNA oligonucleotides exhibit surprisingly good properties with respect to inhibition of the expression of Survivin by means of an anti-sense mechanism, and thereby lead to reduction or inhibition of tumour development in vivo.Type: ApplicationFiled: April 10, 2012Publication date: December 20, 2012Applicant: Santaris Pharma A/SInventors: Christoph Rosenbohm, Lene S. Kjaerulff, Majken Westergaard, Margit Wissenbach, Jens B. Hansen, Marlene Asklund
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Patent number: 8329888Abstract: The present invention is directed to pharmaceutical and therapeutic compositions which comprise RNA complexes comprising an antisense strand and a discontinued passenger strand capable of regulating gene expression. The use of a discontinued passenger strand reduces off target effects of the RNA complexes and also has other advantages.Type: GrantFiled: March 23, 2007Date of Patent: December 11, 2012Assignee: Santaris Pharma A/SInventors: Jesper Wengel, Jorgen Kjems
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Publication number: 20120295955Abstract: The invention relates to oligomer compounds (oligomers), which target HER3 mRNA in a cell, leading to reduced expression of HER3 and/or HER2 and/or EGFR. Reduction of HER3 and/or HER2 and/or EGFR expression is beneficial for a range of medical disorders, such hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of HER3 and/or HER2 and/or EGFR using said oligomers, including methods of treatment.Type: ApplicationFiled: June 22, 2012Publication date: November 22, 2012Applicants: Santaris Pharma A/S, Enzon Pharmaceuticals, Inc.Inventor: Maj Hedtjarn
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Publication number: 20120270924Abstract: Oligonucleotides directed against the hypoxia-inducible factor-1? (HIF-1?) gene are provided for modulating the expression of HIF-1?. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the HIF-1?. Methods of using these compounds for modulation of HIF-1? expression and for the treatment of diseases associated with the hypoxia-inducible factor-1? are provided. Examples of diseases are cancer and pre-eclampsia. The oligonucleotides may be composed of deoxyribonucleosides, a nucleic acid analogue, or Locked Nucleic Acid (LNA) or a combination thereof.Type: ApplicationFiled: May 22, 2012Publication date: October 25, 2012Applicants: Santaris Pharma A/S, Enzon Pharmaceuticals. Inc.Inventors: Charlotte Albæk Thrue, Anja Mølhart Høg, Paul E.G. Kristjansen
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Patent number: 8288356Abstract: The present invention relates to very short heavily modified oligonucleotides which target and inhibit microRNAs in vivo, and their use in medicaments and pharmaceutical compositions.Type: GrantFiled: October 3, 2008Date of Patent: October 16, 2012Assignee: Santaris Pharma A/SInventors: Susanna Obad, Sakari Kauppinen, Joacim Elmen, Morten Lindow, Markus Heidenblad
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Publication number: 20120238618Abstract: The invention provides pharmaceutical compositions comprising short single stranded oligonucleotides, of length of between 8 and 26 nucleobases which are complementary to human microRNAs selected from the group consisting of miR19b, miR21, miR122a, miR155 and miR375. The short oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogues into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the miRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC.Type: ApplicationFiled: March 8, 2012Publication date: September 20, 2012Applicant: Santaris Pharma A/SInventors: Joacim Elmén, Phil Kearney, Sakari Kauppinen
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Patent number: 8268793Abstract: The invention relates to oligomer compounds (oligomers), which target HER3 mRNA in a cell, leading to reduced expression of HER3 and/or HER2 and/or EGFR. Reduction of HER3 and/or HER2 and/or EGFR expression is beneficial for a range of medical disorders, such hyperproliferative disorders (e.g., cancer). The invention provides therapeutic compositions comprising oligomers and methods for modulating the expression of HER3 and/or HER2 and/or EGFR using said oligomers, including methods of treatment.Type: GrantFiled: May 9, 2008Date of Patent: September 18, 2012Assignees: Santaris Pharma A/S, Enzon Pharmaceuticals, Inc.Inventor: Maj Hedtjarn
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Publication number: 20120165514Abstract: The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as ?-L-oxy-LNA, amino-LNA, ?-L-amino-LNA, thio-LNA, ?-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.Type: ApplicationFiled: December 23, 2011Publication date: June 28, 2012Applicant: Santaris Pharma A/SInventors: Mads Detlef Sørensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
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Patent number: 8207140Abstract: Oligonucleotides directed against the hypoxia-inducible factor-1? (HIF-1?) gene are provided for modulating the expression of HIF-1?. The compositions comprise oligonucleotides, particularly antisense oligonucleotides, targeted to nucleic acids encoding the HIF-1?. Methods of using these compounds for modulation of HIF-1? expression and for the treatment of diseases associated with the hypoxia-inducible factor-1? are provided. Examples of diseases are cancer and pre-eclampsia. The oligonucleotides may be composed of deoxyribonucleosides, a nucleic acid analogue, or Locked Nucleic Acid (LNA) or a combination thereof.Type: GrantFiled: October 27, 2010Date of Patent: June 26, 2012Assignees: Santaris Pharma A/S, Enzon Pharmaceuticals, Inc.Inventors: Charlotte Albaek Thrue, Anja Molhart Hog, Paul E. G. Kristjansen
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Publication number: 20120115924Abstract: The present invention relates to the modulation of immunoregulatory proteins, including cytokines, such as colony stimulatory factors (CSF) via the use of microRNA-155 modulators.Type: ApplicationFiled: July 24, 2009Publication date: May 10, 2012Applicant: Santaris Pharma A/SInventors: Jesper Worm, Jan Stenvang, Susanna Obad, Sakari Kauppinen
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Patent number: 8173428Abstract: The present disclosure concerns LNA oligonucleotides having a (sub)sequence of the general formula 5?-(MeCx)(Tx)MeCxAsAstscscsastsgsgsMeCxAx(Gx)(c)-3?, and preferably of the general formula 5?-MeCxTxMeCxAsastscscsastsgsgsMeCxAxGxc-3?, wherein capital letters designate an LNA nucleotide analogue selected from ?-D-oxy-LNA, ?-D-thio-LNA, ?-D-amino-LNA and ?-L-oxy-LNA, small letters designate a deoxynucleotide, and underline designates either an LNA nucleotide analogue as defined above or a deoxynucleotide. Such LNA oligonucleotides exhibit surprisingly good properties with respect to inhibition of the expression of Survivin by means of an anti-sense mechanism, and thereby lead to reduction or inhibition of tumor development in vivo.Type: GrantFiled: October 10, 2008Date of Patent: May 8, 2012Assignees: Santaris Pharma A/S, Enzon Pharmaceuticals, Inc.Inventors: Christoph Rosenbohm, Lene Sonderbye Kjaerulff, Majken Westergaard, Margit Wissenbach, Jens Bo Hansen, Marlene Asklund